Abstract:

The application of chitosan-based surfactants in biomedicine and daily chemicals are progressively increasing for their feature of non-toxic and biodegradable. The micelles formed by amphiphilic modified chitosan can solubilize water-insoluble drugs, slow the drug release, reduce the cytotoxicity and improve the bioavailability of drugs. This paper reviews the researches on the surface activity of chitosan derivatives and their application in drug solubilization and drug carrier. The recent studies on coupling, alkylation, acylation, carboxymethyl-based, quaternary ammonium derivatives of chitosan, and on the drug solubilization of paclitaxel, camptothecin, doxorubicin and methyl-amino folic acid by chitosan-based surfactants are introduced in detail. In the new method of modified chitosan, two ways are worth to notice. The first is to use hydrophobic interactions to constitute the self-assembly system, the second is to introduce the functional groups to form the intelligent drug-loaded micelles.

摘要：

壳聚糖基表面活性剂具有安全无毒和可生物降解等特点，在生物医药和日用化工等行业的应用日益增多。通过双亲性改性获得具有表面活性的壳聚糖所形成的胶束，可以增加难溶药物的溶解度，延长释药时间，提高药物利用率，降低细胞毒性，在药物载体方面具有广阔的应用前景。本文综述了近年来偶联、烷基化、酰基化、羧甲化、季铵化等改性壳聚糖衍生物的表面活性研究以及对紫杉醇、喜树碱、阿霉素和甲氨基叶酸等药物的增溶应用进展。在壳聚糖的改性新方法中有两点值得注意：一是利用疏水相互作用构成自组装体；二是引入具有特殊功能的基团制备智能载药胶束。